Agouron Pharmaceuticals, Inc.

Alanex Corporation

Richard A Bychowski

Min Teng

Yufeng Hong

Daljit Singh Dhanoa

Vlad Edward Gregor

Dilip Ramakant Bhumralkar

Anthony Lai Ling

Javier Gonzalez

Michael David Johnson

Larry Kenneth Truesdale

Atsuo Kuki

Dan Kiel

Ranjan Jagath Rajapakse

Aleksandr K Rabinovich

Dale S Dhanoa

Tso-sheng Chou

David R Luthin

Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.

Non-peptide antagonists of GLP-1 receptor and methods of use

Benzo(e)perimidine-4-carboxamide derivatives of general structural formula I ##STR1## (where R.sub.a, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are as defined in the specification) have activity for receptors of corticotropin releasing factor (CRF). The compounds are useful in treating stress-related diseases, cardiovascular, neurological and psychiatric disorders including anxiety, depression, eating disorders, anorexia nervosa, superanuclear palsy, irritable bowel syndrome, gastrointestinal diseases, immune suppression, inflammatory disorders, drug and alcohol withdrawal symptoms, drug addiction, Alzheimer's disease or fertility disorders.

Benzoperimidine-carboxylic acids and derivatives thereof

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Cardiff, CA, United States of America

Richard A Bychowski